original articleIn vitro screening of reversible and time-dependent inhibition on CYP3A by TM208 and TM209 in rat liver microsomes
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Graphical abstract
This research first demonstrated weak reversible and moderate time-dependent inhibition of two anti-cancer compounds TM208 and TM209 on CYP3A in rat hepatic microsome.
Abbreviations
TM208
4-methylpiperazine-1-carbodithioc acid 3-cyano-3,3-diphenylpropyl ester hydrochloride
TM209
piperazine-1-carbodithioc acid 3-cyano-3,3-diphenylpropyl ester hydrochloride
RLM
rat liver microsome
DDI
drug–drug interaction
CYP
cytochrome P450
DMSO
dimethyl sulfoxide
TDI
time-dependent inhibition
LLOQ
low limit of quantification
PK
pharmacokinetic(s)
Key words
TM208
TM209
RLMs
CYP3A
Reversible inhibition
TDI
DDI
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